So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Ledneczki, Istvan; Tapolcsanyi, Pal; Gabor, Eszter; Visegrady, Andras; Vass, Marton; Eles, Janos; Holm, Patrik; Horvath, Anita; Pocsai, Aniko; Maho, Sandor; Greiner, Istvan; Kramos, Balazs; Beni, Zoltan; Koti, Janos; Kancz, Anna E.; Than, Marta; Kolok, Sandor; Laszy, Judit; Balazs, Ottilia; Bugovits, Gyula; Nagy, Jozsef; Vastag, Monika; Szajli, Agota; Bozo, Eva; Levay, Gyorgy; Lendvai, Balazs; Nemethy, Zsolt researched the compound: 2-Bromomethyl-1,3-dioxolane( cas:4360-63-8 ).Reference of 2-Bromomethyl-1,3-dioxolane.They published the article 《Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach》 about this compound( cas:4360-63-8 ) in European Journal of Medicinal Chemistry. Keywords: pos allosteric modulator nicotinic acetylcholine receptor drug discovery; Cognitive improvement; Nicotinic alpha 7 receptor; Positive allosteric modulator; Scaffold hopping; Structure activity relationship. We’ll tell you more about this compound (cas:4360-63-8).
The paper focuses on the scaffold hopping-based discovery and characterization of novel nicotinic alpha 7 receptor pos. modulator (α7 nAChR PAM) ligands around the reference mol. (A-867744). First, substantial efforts were carried out to assess the importance of the various pharmacophoric elements on the in vitro potency (SAR evaluation) by chem. modifications. Subsequently, several new derivatives with versatile, heteroaromatic central cores were synthesized and characterized. A promising, pyrazole-containing new chemotype with good physicochem. and in vitro parameters was identified. Retrospective anal. based on homol. modeling was also carried out. Besides its favorable in vitro characteristics, the most advanced derivative 69 also showed in vivo efficacy in a rodent model of cognition (scopolamine-induced amnesia in the mouse place recognition test) and acceptable pharmacokinetic properties. Based on the in vivo data, the resulting mol. with advanced drug-like characteristics has the possibility to improve cognitive performance in a biol. relevant dose range, further strengthening the view of the supportive role of α7 nACh receptors in the cognitive processes.
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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem